Patent classifications
C07D213/02
Inhibitors of histone demethylases
The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form ##STR00001##
1,3,4-OXADIAZOLE AMIDE DERIVATIVE COMPOUND AS HISTONE DEACETYLASE 6 INHIBITOR, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases, including infectious diseases; neoplasms; endocrine, nutritional and metabolic diseases; mental and behavioral disorders; neurological diseases; diseases of the eye and adnexa; cardiovascular diseases; respiratory diseases; digestive diseases; diseases of the skin and subcutaneous tissue; diseases of the musculoskeletal system and connective tissue; or congenital malformations, deformations and chromosomal abnormalities.
Process for the preparation of intermediate of dolutegravir
The present invention provides a novel processes for preparation of methyl 3-(benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyiridine-2-carboxylate using novel intermediates.
Abiraterone derivatives and non-covalent complexes with albumin
The present disclosure provides derivatives of abiraterone, non-covalently bound complexes of the abiraterone derivatives with serum albumin, pharmaceutical compositions of the same, and methods of use thereof. The non-covalently bound complexes are significantly more water-soluble than abiraterone and are useful for the treatment of a disease or condition that can benefit from CYP17 inhibition, such as prostate cancer.
ANTI-VIRAL COMPOUNDS
This invention relates to compounds that can be used to treat viral infections. The compounds are papain-like protease (PLpro) inhibitors.
ANTI-VIRAL COMPOUNDS
This invention relates to compounds that can be used to treat viral infections. The compounds are papain-like protease (PLpro) inhibitors.
Organic electroluminescent materials and devices
A luminescent compound that is a metal complex with ligands containing pyrrole or indole in the structure, where the pyrrole or indole has an aromatic substituent that has at least one ortho substitution is disclosed.
Organic electroluminescent materials and devices
A luminescent compound that is a metal complex with ligands containing pyrrole or indole in the structure, where the pyrrole or indole has an aromatic substituent that has at least one ortho substitution is disclosed.
Organometallic Complex, Light-Emitting Element, Light-Emitting Device, Display Device, Electronic Device, and Lighting Device
A novel organometallic complex with high color purity is provided. An organometallic complex represented by General Formula (G1) includes iridium and a plurality of ligands each having a 2-phenylpyridine skeleton, and one or two of the ligands have a carbazole skeleton at the 4-position of the 2-phenylpyridine skeleton.
##STR00001##
(In the formula, R.sup.1 to R.sup.8 and R.sup.9 to R.sup.23 separately represent hydrogen, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted aryl group having 6 to 13 carbon atoms, or a substituted or unsubstituted heteroaryl group having 3 to 12 carbon atoms, and m is 1 or 2.)
PROLYL HYDROXYLASE INHIBITORS
Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.